Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?
- 8 August 2006
- journal article
- review article
- Published by Wiley in FEBS Letters
- Vol. 580 (23), 5492-5499
- https://doi.org/10.1016/j.febslet.2006.07.082
Abstract
The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome.Keywords
This publication has 72 references indexed in Scilit:
- Nuclear Receptor-Dependent Bile Acid Signaling Is Required for Normal Liver RegenerationScience, 2006
- Farnesoid X receptor is essential for normal glucose homeostasisJCI Insight, 2006
- Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasisCell Metabolism, 2005
- Transient impairment of the adaptive response to fasting in FXR‐deficient miceFEBS Letters, 2005
- A mouse genetic model for familial cholestasis caused by ATP8B1 mutations reveals perturbed bile salt homeostasis but no impairment in bile secretionHuman Molecular Genetics, 2004
- The Farnesoid X-receptor Is an Essential Regulator of Cholesterol HomeostasisJournal of Biological Chemistry, 2003
- Regulation of ATP-binding Cassette Sterol Transporters ABCG5 and ABCG8 by the Liver X Receptors α and βJournal of Biological Chemistry, 2002
- The RXR heterodimers and orphan receptorsCell, 1995
- Homozygous disruption of the murine MDR2 P-glycoprotein gene leads to a complete absence of phospholipid from bile and to liver diseaseCell, 1993
- Different Effects of Chenodeoxycholic Acid and Ursodeoxycholic Acid on Serum Lipoprotein Concentrations in Patients with Radiolucent GallstonesScandinavian Journal of Gastroenterology, 1982